Synthesis and preliminary pharmacological evaluation of N-2-(4-(4-(2-substitutedthiazol-4-yl) piperazin-1-yl)-2-oxoethyl)acetamides as novel atypical antipsychotic agents.
A series of N-2-(4-(4-(2-substitutedthiazol-4-yl) piperazin-1-yl)-2-oxoethyl)acetamides were synthesized in an effort to prepare novel atypical antipsychotic agents. The compounds were synthesized by either microwave irradiation technique or by conventional synthesis and were characterized by spectral data (IR, (1)H NMR, and MS) and the purity was ascertained by microanalysis. All the synthesized compounds were screened for their in vivo pharmacological activity in Swiss albino mice. D(2) antagonism studies were performed using climbing mouse assay model and 5-HT(2A) antagonism studies were performed using quipazine induced head twitches in mice. It was observed that none of the new chemical entities exhibited catalepsy. AG 3 was found to be the most active compound.
Sekhar
K V G Chandra
KV
Chemistry Group, Birla Institute of Technology & Science, FDIII, Vidya Vihar, Pilani, Rajasthan 333 031, India. kvgcs@yahoo.com
Rao
V S
VS
Devambatla
Ravi Kumar Vyas
RKV
Kumar
M Murali Krishna
MM
D000081:Acetamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D014150:Antipsychotic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020650:Combinatorial Chemistry Techniques; D004195:Disease Models, Animal; D019416:Head Movements / Q000187:drug effects; D051379:Mice; D015394:Molecular Structure; D009043:Motor Activity / Q000187:drug effects; D010879:Piperazines / Q000138:chemical synthesis* / Q000302:isolation & purification / Q000494:pharmacology*; D011814:Quipazine / Q000494:pharmacology; D058830:Serotonin 5-HT2 Receptor Antagonists
D000081:Acetamides; D014150:Antipsychotic Agents; D010879:Piperazines; D058830:Serotonin 5-HT2 Receptor Antagonists; D011814:Quipazine